Disarib |CAS:1998149-15-7 Probechem Biochemicals

Chemical Structure : Disarib

Disarib (BCL2-BAK inhibitor Disarib)

Catalog No.: PC-62553Not For Human Use, Lab Use Only.

Disarib is a novel BCL2-specific inhibitor that binds predominantly to the BH1 domain, demonstrates strong affinity to BCL2, but not to other antiapoptotic BCL2 family members(BCL-xL, BCL2A1 etc.).

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Biological Activity

Disarib is a novel BCL2-specific inhibitor that binds predominantly to the BH1 domain, demonstrates strong affinity to BCL2, but not to other antiapoptotic BCL2 family members (BCL-xL, BCL2A1 etc.).

Disarib is a novel BCL2 inhibitor with a unique mechanism of BCL2 inhibition.

Disarib shows selective cytotoxicity in BCL2 high cancer cell lines, and CLL patient primary cells, as compared to BCL2 low cell lines.

Disarib induces apoptosis by disruption of BCL2-BAK interaction with Ki of 12.76 nM, but not that of BCL2-BAX or other members of the proapoptotic family such as PUMA and BIM, in vitro.

Disarib abrogates tumor growth while sparing platelets, by activating intrinsic pathway of apoptosis.

Physicochemical Properties

M.Wt	547.855
Formula	C26H16BrClN4OS
Appearance	Solid
CAS No.
Storage	Solide Powder -20 °C 12 Months; 4°C 6 Months	In Solvent -80 °C 6 Months; -20°C 6 Months
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	3-((2-(4-chlorobenzyl)-6-(4-bromophenyl)imidazo[2,1-b][1,3,4] -thiadiazol-5-yl)methylidene)-1,3-dihydro-2H-indol-2-one

References

1. Iyer D, et al. FEBS J. 2016 Sep;283(18):3408-37.

2. Vartak SV, et al. Biochem Pharmacol. 2016 Dec 15;122:10-22.

3. Vartak SV, et al. Biochem Pharmacol. 2017 May 1;131:16-28. doi:

Disarib (BCL2-BAK inhibitor Disarib)

Biological Activity

Physicochemical Properties

References

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